A ring-closing metathesis approach toward formal total synthesis of (+)-diplodialide A.

An asymmetric formal total synthesis of diplodialide A 1a has been achieved starting from methyl acetoacetate 6 and (R)-3-buten-2-ol 7. The macrocyclic ring core of (+)-diplodialide A 1a was constructed, in an excellent yield, by using a ring-closing metathesis strategy.